From [(11)C]CO2 to [(11)C]amides: a rapid one-pot synthesis via the Mitsunobu reaction

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Abstract

A novel amide synthesis methodology is described using amines, CO2 and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [(11)C]CO2. The synthetic utility of the one-pot labelling methodology was demonstrated by producing [(11)C]melatonin. The incorporation of [(11)C]CO2 into [(11)C]melatonin was 36% - determined by radioHPLC 2 min post [(11)C]CO2 delivery.

Original languageEnglish
Pages (from-to)5334-5337
Number of pages4
JournalChemical communications (Cambridge, England)
Volume53
Issue number38
Early online date27 Apr 2017
DOIs
Publication statusE-pub ahead of print - 27 Apr 2017

Keywords

  • Journal Article

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